1. Apoptosis
  2. Bcl-2 Family

Bcl-2 Family

Bcl-2 is a family of evolutionarily related proteins. These proteins govern mitochondrial outer membrane permeabilization (MOMP) and can be either pro-apoptotic (Bax, Bad, Bak and Bok among others) or anti-apoptotic (including Bcl-2 proper, Bcl-xL, and Bcl-w, among an assortment of others). There are a total of 25 genes in the Bcl-2 family known to date. Human genes encoding proteins that belong to this family include: Bak1, Bax, Bal-2, Bok, Mcl-1.

View Bcl-2 Family Pathway Map

Bcl-2 Family 相关产品 (43):

Cat. No. Product Name Effect Purity
  • HY-15531
    ABT-199 Inhibitor 99.80%
    ABT-199 是一种口服有效的 Bcl-2 选择性抑制剂,Ki 值小于 0.01 nM。
  • HY-10087
    Navitoclax Inhibitor 99.80%
    Navitoclax 是一种有效的,可口服的 Bcl-2 抑制剂,对抗凋亡 Bcl-2 蛋白家族 (包括Bcl-xL,Bcl-2 和 Bcl-w) 具有高亲和力,Ki 值小于 1 nM。
  • HY-100741
    S63845 Inhibitor 99.85%
    S63845是高效选择的骨髓细胞白血病1 (MCL1) 抑制剂;结合MCL1的Kd值为0.19 nM。
  • HY-50907
    ABT-737 Inhibitor 98.38%
    ABT-737 是一种类似 BH3 的 Bcl-xLBcl-2Bcl-w 的抑制剂,EC50 值分别为 78.7 nM,30.3 nM 和 197.8 nM;ABT-737 对 Mcl-1,Bcl-B 或 Bfl-1 没有抑制作用。
  • HY-12468
    A-1210477 Inhibitor 98.89%
    A-1210477 是一种有效的,选择性的 MCL-1 抑制剂,较弱地作用于 BCL-2 和 BCL-XL,Ki 值分别为 0.45 nM,132 nM 和 >660 nM。
  • HY-112416
    AZD4320 Inhibitor
    AZD4320 是 BH-3 的新型类似物,有效的 BCL2/BCLxL 的双重抑制剂。AZD4320 对于 KPUM-MS3,KPUM-UH1,和 STR-428 细胞系的 IC50 分别为 26 nM,17 nM,和 170 nM。
  • HY-101778
    ML311 Inhibitor
    ML311 是 Mcl-1/Bim 蛋白之间相互作用的有效选择性抑制剂。
  • HY-N1423
    Glycocholic acid
    Glycocholic acid 是具有抗肿瘤活性的胆汁酸,可靶向作用于耐药泵和非耐药泵通路。
  • HY-10969
    Obatoclax Antagonist 99.20%
    Obatoclax 是一种 BCL-2 家族拮抗剂,结合 BCL-2Ki 约为 220 nM。 Obatoclax 抑制所有 BCL-XL,MCL-1,BCL-w,A1 和 BCL-b 的相互作用 (Ki≈1-7 μM)。
  • HY-15607A
    WEHI-539 hydrochloride Inhibitor
    WEHI-539 hydrochloride 是一种选择性的 Bcl-XL 抑制剂,IC50 为 1.1 nM。
  • HY-19725
    A-1155463 Inhibitor 98.55%
    A-1155463是高效选择性的BCL-XL抑制剂,在Molt-4细胞中的EC50值为70 nM。
  • HY-19741
    A-1331852 Inhibitor 99.21%
    A-1331852是具有口服活性的BCL-XL选择性抑制剂,Ki值小于10 pM。
  • HY-P0081
    Bax inhibitor peptide V5 Inhibitor 99.79%
    Bax inhibitor peptide V5 是一种 Bax 诱导凋亡的抑制剂,主要用于癌症研究。
  • HY-N0087
    Gambogic Acid Inhibitor
    Gambogic acid 来自 Garcinia hanburyi 树的藤黄树脂。Gambogic acid 抑制 Bcl-XLBcl-2Bcl-WBcl-BBfl-1Mcl-1IC50 分别为 1.47 μM,1.21 μM,2.02 μM,0.66 μM,1.06 μM 和 0.79 μM。
  • HY-18628
    UMI-77 Inhibitor 98.04%
    UMI-77是一种选择性的 Mcl-1 抑制剂,对 Mcl-1 具有高亲和力 (IC50= 0.31 μM)。UMI-77 结到 Mcl-1 的 BH3 结合沟, Ki 值为 490 nM,比作用于 Bcl-2 家族其他成员的选择性高。
  • HY-17510
    Gossypol acetic acid Inhibitor 99.42%
    Gossypol acetic acid 是一种从棉籽和根中分离出来的天然产物,分别与 Bcl-xL 蛋白和 Bcl-2 蛋白结合,Ki 值分别为 0.5-0.6 μM 和 0.2-0.3 mM。
  • HY-102027
    FX1 Inhibitor >98.0%
    FX1 是一种强效且特异性的 BCL6 抑制剂, IC50 大约为 35 μM。
  • HY-15464A
    AT-101 acetic acid Inhibitor
    AT-101 acetic acid 是天然产物 Gossypol 的左旋异构体。AT-101 结合到 Bcl-2Mcl-1Bcl-xL 蛋白,Ki 值分别为 260±30 nM,170±10 nM 和 480±40 nM。
  • HY-12011
    HA14-1 Inhibitor >98.0%
    HA14-1 是一种 Bcl-2/Bcl-xL 拮抗剂。HA14-1 与 Bcl-2 上的特定口袋结合, IC50 约为 9 μM,并抑制 Bcl-2 功能。
  • HY-12020
    TW-37 Inhibitor 98.50%
    TW-37 是一种有效的 Bcl-2 抑制剂,作用于 Mcl-1Bcl-2Bcl-xLKi 值分别为 260,290 和 1110 nM。
bcl-2-family-map.png

Bcl-2 family members have been grouped into three classes. The anti-apoptotic subfamily contains the Bcl-2, Bcl-XL, Bcl-w, Mcl-1, Bfl1/A-1, and Bcl-B proteins, which suppress apoptosis and contain all four Bcl-2 homology domains, designated BH1-4. The pro-apoptotic subfamily contain BH1-3 domains, such as Bax, Bak, and Bok. A third class of BH3 only proteins Bad, Bid, Bim, Noxa and Puma have a conserved BH3 domain that can bind and regulate the anti-apoptotic BCL-2 proteins to promote apoptosis [1].


The intrinsic pathway is initiated by various signals, principally extracellular stimuli. BH3-only proteins (Bim, Bid, Bad, Noxa, Puma) engage with anti-apoptotic Bcl-2 family proteins to relieve their inhibition of Bax and Bak to activate them. Next, Bax and Bak are oligomerized and activated, leading to mitochondrial outer membrane permeabilization. Once mitochondrial membranes are permeabilized, cytochrome c and/or Smac/DIABLO is released into the cytoplasm, wherein they combine with an adaptor molecule, Apaf-1, and an inactive initiator Caspase, Pro-caspase 9, within a multiprotein complex called the apoptosome. Smac/DIABLO inhibits IAPs to activate Caspase 9. Caspase 9 activates Caspase 3, which is the initiation step for the cascade of Caspase activation. The extrinsic pathway can be activated by cell surface receptors, such as Fas and TNF Receptor, subsequently activating Caspase 8, and leads to Caspase 3 activation and cell demolition. Caspases in turn cleave a series of substrates, activate DNases and orchestrate the demolition of the cell. Bcl-2 family proteins are also found on the endoplasmic reticulum and the perinuclear membrane in hematopoietic cells, but they are predominantly localized to mitochondria [2]

 

Reference:
[1]. Cotter TG, et al. Apoptosis and cancer: the genesis of a research field. Nat Rev Cancer. 2009 Jul;9(7):501-7.

[2]. Kang MH, et al. Bcl-2 inhibitors: targeting mitochondrial apoptotic pathways in cancer therapy. Clin Cancer Res. 2009 Feb 15;15(4):1126-32.

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